Identification

Name
Theophylline
Accession Number
DB00277  (APRD00082, DB09359)
Type
Small Molecule
Groups
Approved
Description

A methylxanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Mechanistically, theophylline acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Theophylline is marketed under several brand names such as Uniphyl and Theochron, and it is indicated mainly for asthma, bronchospasm, and COPD.

Structure
Thumb
Synonyms
  • 1,3-dimethyl-7H-purine-2,6-dione
  • 1,3-dimethylxanthine
  • Theophyllin
  • Theophylline anhydrous
  • Theophylline, anhydrous
Product Ingredients
IngredientUNIICASInChI Key
Theophylline sodium glycinate2S36N8T7538000-10-0AIJQWRAOMFRHTQ-UHFFFAOYSA-M
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Elixir De TheophyllineElixir80 mgOralLaboratoire Atlas Inc1985-12-31Not applicableCanada
PMS-theophylline ElixirElixir80 mgOralPharmascience Inc1983-12-312016-10-28Canada
Pulmophylline ElxElixir80 mgOralLaboratoire Riva Inc1979-12-31Not applicableCanada
Quibron T SR Tab 300mgTablet, extended release300 mgOralBristol Labs Division Of Bristol Myers Squibb1982-12-312004-08-05Canada
Slo-bid 100Capsule, extended release100 mgOralAventis Pharma Ltd.1987-12-312003-07-22Canada
Slo-bid 200Capsule, extended release200 mgOralAventis Pharma Ltd.1987-12-312003-07-22Canada
Slo-bid 300Capsule, extended release300 mgOralAventis Pharma Ltd.1987-12-312002-07-29Canada
Slo-bid 50Capsule, extended release50 mgOralAventis Pharma Ltd.1988-12-312003-07-22Canada
Teva-theophylline SRTablet, extended release200 mgOralTeva1996-12-19Not applicableCanada
Teva-theophylline SRTablet, extended release300 mgOralTeva1998-04-16Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-theo ERTablet, extended release400 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-theo ERTablet, extended release600 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-theo-LA Srt 100mgTablet, extended release100 mgOralApotex Corporation1993-12-31Not applicableCanada
Apo-theo-LA Srt 200mgTablet, extended release200 mgOralApotex Corporation1993-12-31Not applicableCanada
Apo-theo-LA Srt 300mgTablet, extended release300 mgOralApotex Corporation1993-12-31Not applicableCanada
ElixophyllinLiquid80 mg/15mLOralAtlantic Biologicals Corps.2009-10-01Not applicableUs
ElixophyllinLiquid80 mg/15mLOralNostrum Laboratories, Inc.2009-10-01Not applicableUs
ElixophyllinLiquid80 mg/15mLOralCaraco Pharma, Inc.2009-10-01Not applicableUs
Theo-24Capsule, extended release200 mg/1OralUcb Inc1998-01-202016-01-07Us50474 0200 01 nlmimage10 cd1de6bf
Theo-24Capsule, extended release300 mg/1OralAvera Mc Kennan Hospital2015-03-24Not applicableUs
International/Other Brands
Quibron-T / Respbid / Slo-Bid / Theo 24 / Theo-Dur / Theodur G
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
I D M Expectorant TabTheophylline (70 mg) + Guaifenesin (100 mg) + Pyrilamine maleate (12 mg) + Potassium Iodide (160 mg)TabletOralRougier Pharma Division Of Ratiopharm Inc1975-12-311999-09-27Canada
Idm TabTheophylline (140 mg) + Pyrilamine maleate (25 mg) + Potassium Iodide (325 mg)TabletOralRougier Pharma Division Of Ratiopharm Inc1977-12-311999-09-27Canada
Ratio-theo-broncTheophylline (7 mg) + Guaifenesin (10 mg) + Pyrilamine maleate (1.2 mg) + Potassium Iodide (16 mg)SyrupOralRatiopharm Inc Division Of Teva Canada Limited1964-12-312015-10-26Canada
SenophyllineTheophylline + CholineKitPhysician Therapeutics Llc2011-07-072016-10-13Us
Tedral TabTheophylline (118 mg) + Ephedrine hydrochloride (24 mg) + Phenobarbital (8 mg)TabletOralParke Davis Division, Warner Lambert Canada Inc.1981-12-311999-08-13Canada
Theophylline 0.8mg and 5% Dextrose InjTheophylline (.8 mg) + Glucose (50 mg)SolutionIntravenousBaxter Laboratories1989-12-312008-11-07Canada
Theophylline 0.8mg/ml In 5% Dextrose InjTheophylline (0.8 mg) + Glucose (5.0 %)SolutionIntravenousHospira, Inc.1986-12-312011-08-05Canada
Theophylline 1.6mg and 5% Dextrose InjTheophylline (1.6 mg) + Glucose (50 mg)SolutionIntravenousBaxter Laboratories1989-12-312008-11-07Canada
Theophylline 4mg and 5% Dextrose InjTheophylline (4 mg) + Glucose (50 mg)SolutionIntravenousBaxter Laboratories1995-12-312005-07-29Canada
Theophylline in DextroseTheophylline (80 mg/100mL) + Glucose (5 g/100mL)Injection, solutionIntravenousB. Braun Medical Inc.1992-08-14Not applicableUs
Categories
UNII
0I55128JYK
CAS number
58-55-9
Weight
Average: 180.164
Monoisotopic: 180.06472552
Chemical Formula
C7H8N4O2
InChI Key
ZFXYFBGIUFBOJW-UHFFFAOYSA-N
InChI
InChI=1S/C7H8N4O2/c1-10-5-4(8-3-9-5)6(12)11(2)7(10)13/h3H,1-2H3,(H,8,9)
IUPAC Name
1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione
SMILES
CN1C2=C(NC=N2)C(=O)N(C)C1=O

Pharmacology

Indication

For the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, such as emphysema and chronic bronchitis.

Structured Indications
Pharmacodynamics

Theophylline, an xanthine derivative chemically similar to caffeine and theobromine, is used to treat asthma and bronchospasm. Theophylline has two distinct actions in the airways of patients with reversible (asthmatic) obstruction; smooth muscle relaxation (i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e., non-bronchodilator prophylactic effects).

Mechanism of action

Theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.

TargetActionsOrganism
AAdenosine receptor A1
antagonist
Human
AAdenosine receptor A2a
antagonist
Human
AAdenosine receptor A2b
antagonist
Human
AcAMP-specific 3',5'-cyclic phosphodiesterase 4B
inhibitor
Human
AcGMP-specific 3',5'-cyclic phosphodiesterase
inhibitor
Human
AcAMP-specific 3',5'-cyclic phosphodiesterase 4A
inhibitor
Human
AcGMP-inhibited 3',5'-cyclic phosphodiesterase A
inhibitor
Human
AHistone deacetylase 2
activator
Human
UCopine-1Not AvailableHuman
UMinor histocompatibility antigen H13Not AvailableHuman
UNodal modulator 1Not AvailableHuman
UPoly [ADP-ribose] polymerase 1Not AvailableHuman
UProtein RIC-3Not AvailableHuman
UTubulin monoglycylase TTLL3Not AvailableHuman
Absorption

Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.

Volume of distribution
  • 0.3 to 0.7 L/kg
Protein binding

40%, primarily to albumin.

Metabolism

Hepatic. Biotransformation takes place through demethylation to 1-methylxanthine and 3-methylxanthine and hydroxylation to 1,3-dimethyluric acid. 1-methylxanthine is further hydroxylated, by xanthine oxidase, to 1-methyluric acid. About 6% of a theophylline dose is N-methylated to caffeine. Caffeine and 3-methylxanthine are the only theophylline metabolites with pharmacologic activity.

Route of elimination

Theophylline does not undergo any appreciable pre-systemic elimination, distributes freely into fat-free tissues and is extensively metabolized in the liver. Renal excretion of unchanged theophylline in neonates amounts to about 50% of the dose, compared to about 10% in children older than three months and in adults.

Half life

8 hours

Clearance
  • 0.29 mL/kg/min [Premature neonates, postnatal age 3-15 days]
  • 0.64 mL/kg/min [Premature neonates, postnatal age 25-57 days]
  • 1.7 mL/kg/min [Children 1-4 years]
  • 1.6 mL/kg/min [Children 4-12 years]
  • 0.9 mL/kg/min [Children 13-15 years]
  • 1.4 mL/kg/min [Children 16-17 years]
  • 0.65 mL/kg/min [Adults (16-60 years), otherwise healthy non-smoking asthmatics]
  • 0.41 mL/kg/min [Elderly (>60 years), non-smokers with normal cardiac, liver, and renal function]
  • 0.33 mL/kg/min [Acute pulmonary edema]
  • 0.54 mL/kg/min [COPD >60 years, stable, non-smoker >1 year]
  • 0.48 mL/kg/min [COPD with cor pulmonale]
  • 1.25 mL/kg/min [Cystic fibrosis (14-28 years)]
  • 0.31 mL/kg/min [Liver disease cirrhosis]
  • 0.35 mL/kg/min [acute hepatitis]
  • 0.65 mL/kg/min [cholestasis]
  • 0.47 mL/kg/min [Sepsis with multi-organ failure]
  • 0.38 mL/kg/min [hypothyroid]
  • 0.8 mL/kg/min [hyperthyroid]
Toxicity

Symptoms of overdose include seizures, arrhythmias, and GI effects.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Caffeine MetabolismMetabolic
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 1A2-2964(G/A)(A;A) / (G;A)A AlleleEffect Directly StudiedPatients with this genotype have reduced metabolism of theophylline.Details

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe serum concentration of Theophylline can be decreased when it is combined with 1,10-Phenanthroline.Experimental
3,4-DichloroisocoumarinThe serum concentration of Theophylline can be decreased when it is combined with 3,4-Dichloroisocoumarin.Experimental
4-(2-Aminoethyl)Benzenesulfonyl FluorideThe serum concentration of Theophylline can be decreased when it is combined with 4-(2-Aminoethyl)Benzenesulfonyl Fluoride.Experimental
AbirateroneThe serum concentration of Theophylline can be increased when it is combined with Abiraterone.Approved
AcebutololAcebutolol may decrease the bronchodilatory activities of Theophylline.Approved
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Theophylline.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Theophylline.Approved
AdalimumabThe serum concentration of Theophylline can be decreased when it is combined with Adalimumab.Approved
AdenosineThe therapeutic efficacy of Adenosine can be decreased when used in combination with Theophylline.Approved, Investigational
AgomelatineThe serum concentration of Agomelatine can be increased when it is combined with Theophylline.Approved, Investigational
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Theophylline.Approved, Vet Approved
Albinterferon Alfa-2BThe metabolism of Theophylline can be decreased when combined with Albinterferon Alfa-2B.Investigational
AllopurinolThe serum concentration of Theophylline can be increased when it is combined with Allopurinol.Approved
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Theophylline.Approved, Investigational
AlogliptinThe serum concentration of Theophylline can be decreased when it is combined with Alogliptin.Approved
AlosetronThe metabolism of Alosetron can be decreased when combined with Theophylline.Approved, Withdrawn
Alpha-1-proteinase inhibitorThe serum concentration of Theophylline can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
AlprazolamThe therapeutic efficacy of Alprazolam can be decreased when used in combination with Theophylline.Approved, Illicit, Investigational
AlprenololAlprenolol may decrease the bronchodilatory activities of Theophylline.Approved, Withdrawn
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Theophylline.Approved, Withdrawn
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Theophylline.Approved
AmiodaroneThe metabolism of Theophylline can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Theophylline.Approved
AmobarbitalThe serum concentration of Theophylline can be decreased when it is combined with Amobarbital.Approved, Illicit
AmprenavirThe serum concentration of Theophylline can be decreased when it is combined with Amprenavir.Approved
AnagrelideThe metabolism of Anagrelide can be decreased when combined with Theophylline.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Theophylline.Approved
Antithrombin III humanThe serum concentration of Theophylline can be decreased when it is combined with Antithrombin III human.Approved
ApixabanThe metabolism of Apixaban can be decreased when combined with Theophylline.Approved
AprepitantThe serum concentration of Theophylline can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe serum concentration of Theophylline can be decreased when it is combined with Aprotinin.Approved, Withdrawn
ArgatrobanThe serum concentration of Theophylline can be decreased when it is combined with Argatroban.Approved, Investigational
ArtemetherThe metabolism of Theophylline can be decreased when combined with Artemether.Approved
AsenapineThe metabolism of Asenapine can be decreased when combined with Theophylline.Approved
AsunaprevirThe serum concentration of Theophylline can be decreased when it is combined with Asunaprevir.Approved, Investigational
AtazanavirThe metabolism of Theophylline can be decreased when combined with Atazanavir.Approved, Investigational
AtenololAtenolol may decrease the bronchodilatory activities of Theophylline.Approved
AtomoxetineThe metabolism of Theophylline can be decreased when combined with Atomoxetine.Approved
AV650The metabolism of AV650 can be decreased when combined with Theophylline.Approved, Investigational
AxitinibThe metabolism of Axitinib can be decreased when combined with Theophylline.Approved, Investigational
AzelastineThe metabolism of Azelastine can be decreased when combined with Theophylline.Approved
AzithromycinThe metabolism of Theophylline can be decreased when combined with Azithromycin.Approved
BarbexacloneThe serum concentration of Theophylline can be decreased when it is combined with Barbexaclone.Experimental
BarbitalThe serum concentration of Theophylline can be decreased when it is combined with Barbital.Illicit
BatimastatThe serum concentration of Theophylline can be decreased when it is combined with Batimastat.Experimental
BenazeprilThe serum concentration of Theophylline can be decreased when it is combined with Benazepril.Approved, Investigational
BendamustineThe metabolism of Bendamustine can be decreased when combined with Theophylline.Approved, Investigational
BenzamidineThe serum concentration of Theophylline can be decreased when it is combined with Benzamidine.Experimental
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Theophylline.Approved
BetaxololThe metabolism of Betaxolol can be decreased when combined with Theophylline.Approved
BisoprololBisoprolol may decrease the bronchodilatory activities of Theophylline.Approved
BivalirudinThe serum concentration of Theophylline can be decreased when it is combined with Bivalirudin.Approved, Investigational
BMS-906024The therapeutic efficacy of BMS-906024 can be decreased when used in combination with Theophylline.Investigational
BoceprevirThe metabolism of Theophylline can be decreased when combined with Boceprevir.Approved, Withdrawn
BopindololBopindolol may decrease the bronchodilatory activities of Theophylline.Approved
BortezomibThe metabolism of Theophylline can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Theophylline can be decreased when it is combined with Bosentan.Approved, Investigational
BromazepamThe therapeutic efficacy of Bromazepam can be decreased when used in combination with Theophylline.Approved, Illicit
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Theophylline.Approved, Investigational
BupranololBupranolol may decrease the bronchodilatory activities of Theophylline.Approved
BupropionThe metabolism of Theophylline can be decreased when combined with Bupropion.Approved
CaffeineThe metabolism of Theophylline can be decreased when combined with Caffeine.Approved
CamazepamThe therapeutic efficacy of Camazepam can be decreased when used in combination with Theophylline.Approved, Illicit
CamostatThe serum concentration of Theophylline can be decreased when it is combined with Camostat.Experimental
CandoxatrilThe serum concentration of Theophylline can be decreased when it is combined with Candoxatril.Experimental
CandoxatrilatThe serum concentration of Theophylline can be decreased when it is combined with Candoxatrilat.Experimental
CapecitabineThe metabolism of Theophylline can be decreased when combined with Capecitabine.Approved, Investigational
CaptoprilThe serum concentration of Theophylline can be decreased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Theophylline can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarbimazoleThe serum concentration of Theophylline can be increased when it is combined with Carbimazole.Approved, Investigational
CarbomycinThe metabolism of Theophylline can be decreased when combined with Carbomycin.Vet Approved
CarmustineThe metabolism of Carmustine can be decreased when combined with Theophylline.Approved
CarteololCarteolol may decrease the bronchodilatory activities of Theophylline.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Theophylline.Approved, Investigational
CE-326597The therapeutic efficacy of CE-326597 can be decreased when used in combination with Theophylline.Investigational
CelecoxibThe metabolism of Theophylline can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololCeliprolol may decrease the bronchodilatory activities of Theophylline.Approved, Investigational
Cepeginterferon alfa-2BThe metabolism of Theophylline can be decreased when combined with Cepeginterferon alfa-2B.Investigational
CeritinibThe serum concentration of Theophylline can be increased when it is combined with Ceritinib.Approved
ChlordiazepoxideThe therapeutic efficacy of Chlordiazepoxide can be decreased when used in combination with Theophylline.Approved, Illicit
ChloroquineThe metabolism of Theophylline can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Theophylline can be increased when it is combined with Chlorotrianisene.Investigational, Withdrawn
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Theophylline.Approved, Vet Approved
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Theophylline.Approved
CholecalciferolThe metabolism of Theophylline can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Theophylline can be decreased when it is combined with Cholesterol.Experimental, Investigational
ChymostatinThe serum concentration of Theophylline can be decreased when it is combined with Chymostatin.Experimental
CilastatinThe serum concentration of Theophylline can be decreased when it is combined with Cilastatin.Approved
CilazaprilThe serum concentration of Theophylline can be decreased when it is combined with Cilazapril.Approved
CilostazolThe metabolism of Cilostazol can be decreased when combined with Theophylline.Approved
CimetidineThe metabolism of Theophylline can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Theophylline can be decreased when combined with Cinacalcet.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Theophylline.Approved, Investigational
CinoxacinThe metabolism of Theophylline can be decreased when combined with Cinoxacin.Approved, Investigational, Withdrawn
CisaprideThe metabolism of Cisapride can be decreased when combined with Theophylline.Approved, Investigational, Withdrawn
CitalopramThe metabolism of Theophylline can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Theophylline can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Theophylline can be decreased when combined with Clemastine.Approved
ClenbuterolThe metabolism of Clenbuterol can be decreased when combined with Theophylline.Approved, Investigational, Vet Approved
ClevidipineThe metabolism of Clevidipine can be decreased when combined with Theophylline.Approved
ClobazamThe therapeutic efficacy of Clobazam can be decreased when used in combination with Theophylline.Approved, Illicit
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Theophylline.Approved, Vet Approved
ClonazepamThe therapeutic efficacy of Clonazepam can be decreased when used in combination with Theophylline.Approved, Illicit
ClonidineThe metabolism of Clonidine can be decreased when combined with Theophylline.Approved
ClopidogrelThe metabolism of Clopidogrel can be decreased when combined with Theophylline.Approved, Nutraceutical
CloranololCloranolol may decrease the bronchodilatory activities of Theophylline.Experimental
ClorazepateThe therapeutic efficacy of Clorazepate can be decreased when used in combination with Theophylline.Approved, Illicit
ClotrimazoleThe metabolism of Theophylline can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Clozapine can be decreased when combined with Theophylline.Approved
CobicistatThe serum concentration of Theophylline can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Theophylline can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Theophylline can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated estrogensThe metabolism of Conjugated estrogens can be decreased when combined with Theophylline.Approved
CrisaboroleThe metabolism of Theophylline can be decreased when combined with Crisaborole.Approved
CrizotinibThe metabolism of Theophylline can be decreased when combined with Crizotinib.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Theophylline.Approved
CyclosporineThe metabolism of Theophylline can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Theophylline can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateThe serum concentration of Theophylline can be decreased when it is combined with Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Theophylline can be decreased when it is combined with Dabrafenib.Approved
DacarbazineThe metabolism of Dacarbazine can be decreased when combined with Theophylline.Approved, Investigational
DaidzeinThe serum concentration of Theophylline can be increased when it is combined with Daidzein.Experimental
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Theophylline.Approved
DarexabanThe serum concentration of Theophylline can be decreased when it is combined with Darexaban.Investigational
DarifenacinThe metabolism of Theophylline can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Theophylline can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Theophylline can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe metabolism of Daunorubicin can be decreased when combined with Theophylline.Approved
DeferasiroxThe serum concentration of Theophylline can be increased when it is combined with Deferasirox.Approved, Investigational
DelanzomibThe serum concentration of Theophylline can be decreased when it is combined with Delanzomib.Investigational
DelaprilThe serum concentration of Theophylline can be decreased when it is combined with Delapril.Experimental
DelavirdineThe metabolism of Theophylline can be decreased when combined with Delavirdine.Approved
DelorazepamThe therapeutic efficacy of Delorazepam can be decreased when used in combination with Theophylline.Approved, Illicit, Investigational
DesipramineThe metabolism of Desipramine can be decreased when combined with Theophylline.Approved
DeutetrabenazineThe metabolism of Deutetrabenazine can be decreased when combined with Theophylline.Approved, Investigational
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Theophylline.Approved, Illicit, Investigational, Withdrawn
DiazepamThe therapeutic efficacy of Diazepam can be decreased when used in combination with Theophylline.Approved, Illicit, Vet Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Theophylline.Approved, Vet Approved
DienestrolThe serum concentration of Theophylline can be increased when it is combined with Dienestrol.Approved, Investigational
DiethylstilbestrolThe serum concentration of Theophylline can be increased when it is combined with Diethylstilbestrol.Approved, Investigational
DihydroergotamineThe metabolism of Theophylline can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Theophylline can be decreased when combined with Diltiazem.Approved
DinoprostoneThe metabolism of Dinoprostone can be decreased when combined with Theophylline.Approved
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Theophylline.Approved
DisulfiramThe serum concentration of Theophylline can be increased when it is combined with Disulfiram.Approved
DomperidoneThe metabolism of Domperidone can be decreased when combined with Theophylline.Approved, Investigational, Vet Approved
DosulepinThe metabolism of Theophylline can be decreased when combined with Dosulepin.Approved
DoxefazepamThe therapeutic efficacy of Doxefazepam can be decreased when used in combination with Theophylline.Experimental
DoxepinThe metabolism of Doxepin can be decreased when combined with Theophylline.Approved
DoxofyllineThe risk or severity of adverse effects can be increased when Theophylline is combined with Doxofylline.Approved
DoxycyclineThe metabolism of Theophylline can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Theophylline can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Duloxetine can be decreased when combined with Theophylline.Approved
EcabetThe serum concentration of Theophylline can be decreased when it is combined with Ecabet.Approved, Investigational
EdoxabanThe serum concentration of Theophylline can be decreased when it is combined with Edoxaban.Approved
EfavirenzThe metabolism of Theophylline can be decreased when combined with Efavirenz.Approved, Investigational
ElafinThe serum concentration of Theophylline can be decreased when it is combined with Elafin.Investigational
EliglustatThe metabolism of Theophylline can be decreased when combined with Eliglustat.Approved
EltrombopagThe metabolism of Eltrombopag can be decreased when combined with Theophylline.Approved
EnalaprilThe serum concentration of Theophylline can be decreased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe serum concentration of Theophylline can be decreased when it is combined with Enalaprilat.Approved
EnalkirenThe serum concentration of Theophylline can be decreased when it is combined with Enalkiren.Experimental
EnasidenibThe metabolism of Enasidenib can be decreased when combined with Theophylline.Approved
EnoxacinThe metabolism of Theophylline can be decreased when combined with Enoxacin.Approved, Investigational
EnzalutamideThe serum concentration of Theophylline can be decreased when it is combined with Enzalutamide.Approved
Epigallocatechin GallateThe serum concentration of Theophylline can be decreased when it is combined with Epigallocatechin Gallate.Investigational
EpimestrolThe serum concentration of Theophylline can be increased when it is combined with Epimestrol.Experimental
EquolThe serum concentration of Theophylline can be increased when it is combined with Equol.Investigational
ErgotamineThe metabolism of Ergotamine can be decreased when combined with Theophylline.Approved
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Theophylline.Approved, Investigational
ErythromycinThe metabolism of Theophylline can be decreased when combined with Erythromycin.Approved, Vet Approved
EsmololEsmolol may decrease the bronchodilatory activities of Theophylline.Approved
EstazolamThe therapeutic efficacy of Estazolam can be decreased when used in combination with Theophylline.Approved, Illicit
EstradiolThe metabolism of Estradiol can be decreased when combined with Theophylline.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Theophylline can be increased when it is combined with Estriol.Approved, Investigational, Vet Approved
Estrogens, esterifiedThe serum concentration of Theophylline can be increased when it is combined with Estrogens, esterified.Approved
EstroneThe metabolism of Estrone can be decreased when combined with Theophylline.Approved
Estrone sulfateThe metabolism of Estrone sulfate can be decreased when combined with Theophylline.Approved
EthanolThe serum concentration of Theophylline can be increased when it is combined with Ethanol.Approved
Ethinyl EstradiolThe serum concentration of Theophylline can be increased when it is combined with Ethinyl Estradiol.Approved
EtizolamThe therapeutic efficacy of Etizolam can be decreased when used in combination with Theophylline.Approved
EtoposideThe metabolism of Etoposide can be decreased when combined with Theophylline.Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Theophylline.Approved, Investigational
EtravirineThe metabolism of Theophylline can be decreased when combined with Etravirine.Approved
FaldaprevirThe serum concentration of Theophylline can be decreased when it is combined with Faldaprevir.Investigational
FebuxostatThe serum concentration of the active metabolites of Theophylline can be increased when Theophylline is used in combination with Febuxostat.Approved
FelodipineThe metabolism of Theophylline can be decreased when combined with Felodipine.Approved, Investigational
FleroxacinThe metabolism of Theophylline can be decreased when combined with Fleroxacin.Approved
FloxuridineThe metabolism of Theophylline can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Theophylline can be decreased when combined with Fluconazole.Approved
FludiazepamThe therapeutic efficacy of Fludiazepam can be decreased when used in combination with Theophylline.Approved, Illicit
FlumazenilThe therapeutic efficacy of Flumazenil can be decreased when used in combination with Theophylline.Approved
FlumequineThe metabolism of Theophylline can be decreased when combined with Flumequine.Withdrawn
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Theophylline.Approved
FlunitrazepamThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Theophylline.Approved, Illicit
FluorouracilThe metabolism of Theophylline can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Theophylline can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlurazepamThe therapeutic efficacy of Flurazepam can be decreased when used in combination with Theophylline.Approved, Illicit
FlutamideThe metabolism of Flutamide can be decreased when combined with Theophylline.Approved
FluvastatinThe metabolism of Theophylline can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Theophylline can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolThe risk or severity of adverse effects can be increased when Theophylline is combined with Formoterol.Approved, Investigational
FosamprenavirThe metabolism of Theophylline can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Theophylline can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe serum concentration of Theophylline can be decreased when it is combined with Fosinopril.Approved
FosphenytoinThe serum concentration of Theophylline can be decreased when it is combined with Fosphenytoin.Approved
FrovatriptanThe metabolism of Frovatriptan can be decreased when combined with Theophylline.Approved, Investigational
Fusidic AcidThe serum concentration of Theophylline can be increased when it is combined with Fusidic Acid.Approved
GabexateThe serum concentration of Theophylline can be decreased when it is combined with Gabexate.Investigational
GarenoxacinThe metabolism of Theophylline can be decreased when combined with Garenoxacin.Investigational
GatifloxacinThe metabolism of Theophylline can be decreased when combined with Gatifloxacin.Approved, Investigational
GeldanamycinThe serum concentration of Theophylline can be decreased when it is combined with Geldanamycin.Experimental, Investigational
GemfibrozilThe metabolism of Theophylline can be decreased when combined with Gemfibrozil.Approved
GemifloxacinThe metabolism of Theophylline can be decreased when combined with Gemifloxacin.Approved, Investigational
GenisteinThe metabolism of Genistein can be decreased when combined with Theophylline.Investigational
GM6001The serum concentration of Theophylline can be decreased when it is combined with GM6001.Experimental
GrepafloxacinThe metabolism of Theophylline can be decreased when combined with Grepafloxacin.Investigational, Withdrawn
GuanabenzThe metabolism of Guanabenz can be decreased when combined with Theophylline.Approved, Investigational
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Theophylline.Approved
HesperetinThe metabolism of Hesperetin can be decreased when combined with Theophylline.Approved
HexestrolThe serum concentration of Theophylline can be increased when it is combined with Hexestrol.Withdrawn
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Theophylline.Approved
IcotinibThe metabolism of Icotinib can be decreased when combined with Theophylline.Approved, Investigational
IdelalisibThe serum concentration of Theophylline can be increased when it is combined with Idelalisib.Approved
IdraparinuxThe serum concentration of Theophylline can be decreased when it is combined with Idraparinux.Investigational
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Theophylline.Approved
ImatinibThe metabolism of Theophylline can be decreased when combined with Imatinib.Approved
ImidaprilThe serum concentration of Theophylline can be decreased when it is combined with Imidapril.Investigational
ImipramineThe metabolism of Imipramine can be decreased when combined with Theophylline.Approved
ImiquimodThe metabolism of Imiquimod can be decreased when combined with Theophylline.Approved, Investigational
IndacaterolThe risk or severity of adverse effects can be increased when Theophylline is combined with Indacaterol.Approved
IndinavirThe metabolism of Theophylline can be decreased when combined with Indinavir.Approved
Interferon Alfa-2a, RecombinantThe metabolism of Theophylline can be decreased when combined with Interferon Alfa-2a, Recombinant.Approved, Investigational
Interferon Alfa-2b, RecombinantThe metabolism of Theophylline can be decreased when combined with Interferon Alfa-2b, Recombinant.Approved
Interferon alfa-n1The metabolism of Theophylline can be decreased when combined with Interferon alfa-n1.Approved, Investigational
Interferon alfa-n3The metabolism of Theophylline can be decreased when combined with Interferon alfa-n3.Approved, Investigational
Interferon alfacon-1The metabolism of Theophylline can be decreased when combined with Interferon alfacon-1.Approved, Investigational
Interferon beta-1aThe metabolism of Theophylline can be decreased when combined with Interferon beta-1a.Approved, Investigational
Interferon beta-1bThe metabolism of Theophylline can be decreased when combined with Interferon beta-1b.Approved
Interferon gamma-1bThe metabolism of Theophylline can be decreased when combined with Interferon gamma-1b.Approved, Investigational
IrbesartanThe metabolism of Theophylline can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Theophylline can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoflurophateThe serum concentration of Theophylline can be decreased when it is combined with Isoflurophate.Approved, Investigational, Withdrawn
IsoniazidThe serum concentration of Theophylline can be increased when it is combined with Isoniazid.Approved
IsoprenalineThe serum concentration of Theophylline can be decreased when it is combined with Isoprenaline.Approved
IsradipineThe metabolism of Theophylline can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Theophylline can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Theophylline can be increased when it is combined with Ivacaftor.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Theophylline.Approved
JosamycinThe metabolism of Theophylline can be decreased when combined with Josamycin.Approved, Investigational
KetoconazoleThe metabolism of Theophylline can be decreased when combined with Ketoconazole.Approved, Investigational
KitasamycinThe metabolism of Theophylline can be decreased when combined with Kitasamycin.Experimental
LapatinibThe metabolism of Theophylline can be decreased when combined with Lapatinib.Approved, Investigational
LeflunomideThe metabolism of Leflunomide can be decreased when combined with Theophylline.Approved, Investigational
LepirudinThe serum concentration of Theophylline can be decreased when it is combined with Lepirudin.Approved
LetaxabanThe serum concentration of Theophylline can be decreased when it is combined with Letaxaban.Investigational
LevobupivacaineThe metabolism of Levobupivacaine can be decreased when combined with Theophylline.Approved, Investigational
LevofloxacinThe metabolism of Theophylline can be decreased when combined with Levofloxacin.Approved, Investigational
LevothyroxineThe metabolism of Theophylline can be increased when combined with Levothyroxine.Approved
LidocaineThe metabolism of Lidocaine can be decreased when combined with Theophylline.Approved, Vet Approved
LinagliptinThe serum concentration of Theophylline can be decreased when it is combined with Linagliptin.Approved
LiothyronineThe metabolism of Theophylline can be increased when combined with Liothyronine.Approved, Vet Approved
LiotrixThe metabolism of Theophylline can be increased when combined with Liotrix.Approved
LisinoprilThe serum concentration of Theophylline can be decreased when it is combined with Lisinopril.Approved, Investigational
LithiumThe serum concentration of Lithium can be decreased when it is combined with Theophylline.Approved
LobeglitazoneThe metabolism of Theophylline can be decreased when combined with Lobeglitazone.Approved, Investigational
LomefloxacinThe metabolism of Lomefloxacin can be decreased when combined with Theophylline.Approved, Investigational
LopinavirThe metabolism of Theophylline can be decreased when combined with Lopinavir.Approved
LorazepamThe therapeutic efficacy of Lorazepam can be decreased when used in combination with Theophylline.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Theophylline.Approved
LormetazepamThe therapeutic efficacy of Lormetazepam can be decreased when used in combination with Theophylline.Approved
LosartanThe metabolism of Theophylline can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Theophylline can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Theophylline can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Theophylline can be increased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Theophylline can be decreased when combined with Lumefantrine.Approved
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Theophylline.Approved, Investigational
MalathionThe metabolism of Malathion can be decreased when combined with Theophylline.Approved, Investigational
ManidipineThe metabolism of Theophylline can be decreased when combined with Manidipine.Approved, Investigational
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Theophylline.Approved
MedazepamThe therapeutic efficacy of Medazepam can be decreased when used in combination with Theophylline.Experimental
MelagatranThe serum concentration of Theophylline can be decreased when it is combined with Melagatran.Experimental
MelatoninThe metabolism of Melatonin can be decreased when combined with Theophylline.Approved, Nutraceutical, Vet Approved
MenadioneThe metabolism of Menadione can be decreased when combined with Theophylline.Approved, Nutraceutical
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Theophylline.Investigational, Withdrawn
MepindololMepindolol may decrease the bronchodilatory activities of Theophylline.Experimental
MestranolThe serum concentration of Theophylline can be increased when it is combined with Mestranol.Approved
MethadoneThe metabolism of Methadone can be decreased when combined with Theophylline.Approved
MethallenestrilThe serum concentration of Theophylline can be increased when it is combined with Methallenestril.Experimental
MethimazoleThe serum concentration of Theophylline can be increased when it is combined with Methimazole.Approved
MethohexitalThe serum concentration of Theophylline can be decreased when it is combined with Methohexital.Approved
MethotrexateThe serum concentration of Theophylline can be increased when it is combined with Methotrexate.Approved
MethotrimeprazineThe metabolism of Theophylline can be decreased when combined with Methotrimeprazine.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Theophylline.Approved, Investigational, Vet Approved
MethylphenobarbitalThe serum concentration of Theophylline can be decreased when it is combined with Methylphenobarbital.Approved
MethylthiouracilThe serum concentration of Theophylline can be increased when it is combined with Methylthiouracil.Experimental
MetoprololThe metabolism of Theophylline can be decreased when combined with Metoprolol.Approved, Investigational
MetreleptinThe serum concentration of Theophylline can be decreased when it is combined with Metreleptin.Approved
MexiletineThe metabolism of Theophylline can be decreased when combined with Mexiletine.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Theophylline.Approved, Investigational
MidazolamThe therapeutic efficacy of Midazolam can be decreased when used in combination with Theophylline.Approved, Illicit
MidostaurinThe metabolism of Theophylline can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Theophylline can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Theophylline can be decreased when combined with Mirabegron.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Theophylline.Approved
MitotaneThe serum concentration of Theophylline can be decreased when it is combined with Mitotane.Approved
MoexiprilThe serum concentration of Theophylline can be decreased when it is combined with Moexipril.Approved
MoxestrolThe serum concentration of Theophylline can be increased when it is combined with Moxestrol.Experimental
muraglitazarThe metabolism of muraglitazar can be decreased when combined with Theophylline.Investigational
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe serum concentration of Theophylline can be decreased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.Experimental
NabumetoneThe metabolism of Nabumetone can be decreased when combined with Theophylline.Approved
NafamostatThe serum concentration of Theophylline can be decreased when it is combined with Nafamostat.Approved, Investigational
Nalidixic AcidThe metabolism of Theophylline can be decreased when combined with Nalidixic Acid.Approved, Investigational
NaproxenThe metabolism of Naproxen can be decreased when combined with Theophylline.Approved, Vet Approved
Natural alpha interferonThe metabolism of Theophylline can be decreased when combined with Natural alpha interferon.Approved, Investigational
NebivololNebivolol may decrease the bronchodilatory activities of Theophylline.Approved, Investigational
NefazodoneThe metabolism of Theophylline can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Theophylline can be decreased when combined with Nelfinavir.Approved
NemonoxacinThe metabolism of Theophylline can be decreased when combined with Nemonoxacin.Investigational
NetazepideThe therapeutic efficacy of Netazepide can be decreased when used in combination with Theophylline.Investigational
NetupitantThe serum concentration of Theophylline can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Theophylline can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Theophylline can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Theophylline.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Theophylline.Approved
NilotinibThe metabolism of Theophylline can be decreased when combined with Nilotinib.Approved, Investigational
NitrazepamThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Theophylline.Approved
Nitric OxideThe metabolism of Nitric Oxide can be decreased when combined with Theophylline.Approved
NitroaspirinThe serum concentration of Theophylline can be decreased when it is combined with Nitroaspirin.Investigational
NorfloxacinThe metabolism of Theophylline can be decreased when combined with Norfloxacin.Approved
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Theophylline.Approved
OlanzapineThe metabolism of Olanzapine can be decreased when combined with Theophylline.Approved, Investigational
OlaparibThe metabolism of Theophylline can be decreased when combined with Olaparib.Approved
OleandomycinThe metabolism of Theophylline can be decreased when combined with Oleandomycin.Vet Approved
OlodaterolThe risk or severity of adverse effects can be increased when Theophylline is combined with Olodaterol.Approved
OmapatrilatThe serum concentration of Theophylline can be decreased when it is combined with Omapatrilat.Investigational
OmeprazoleThe metabolism of Omeprazole can be decreased when combined with Theophylline.Approved, Investigational, Vet Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Theophylline.Approved
OsimertinibThe serum concentration of Theophylline can be increased when it is combined with Osimertinib.Approved
OtamixabanThe serum concentration of Theophylline can be decreased when it is combined with Otamixaban.Investigational
OxaliplatinThe metabolism of Oxaliplatin can be decreased when combined with Theophylline.Approved, Investigational
OxazepamThe therapeutic efficacy of Oxazepam can be decreased when used in combination with Theophylline.Approved
Oxolinic acidThe metabolism of Theophylline can be decreased when combined with Oxolinic acid.Experimental
OxprenololOxprenolol may decrease the bronchodilatory activities of Theophylline.Approved
OxtriphyllineThe metabolism of Oxtriphylline can be decreased when combined with Theophylline.Approved
PalbociclibThe serum concentration of Theophylline can be increased when it is combined with Palbociclib.Approved
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Theophylline.Approved, Investigational
PancuroniumThe risk or severity of adverse effects can be increased when Theophylline is combined with Pancuronium.Approved
PanobinostatThe serum concentration of Theophylline can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Theophylline.Approved
ParoxetineThe metabolism of Theophylline can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe metabolism of Pazopanib can be decreased when combined with Theophylline.Approved
PazufloxacinThe metabolism of Theophylline can be decreased when combined with Pazufloxacin.Investigational
PefloxacinThe metabolism of Theophylline can be decreased when combined with Pefloxacin.Approved
Peginterferon alfa-2aThe metabolism of Theophylline can be decreased when combined with Peginterferon alfa-2a.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Theophylline can be decreased when it is combined with Peginterferon alfa-2b.Approved
Peginterferon beta-1aThe metabolism of Theophylline can be decreased when combined with Peginterferon beta-1a.Approved
PenbutololPenbutolol may decrease the bronchodilatory activities of Theophylline.Approved, Investigational
PentamidineThe metabolism of Pentamidine can be decreased when combined with Theophylline.Approved
PentobarbitalThe metabolism of Theophylline can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoxifyllineThe serum concentration of Theophylline can be increased when it is combined with Pentoxifylline.Approved, Investigational
PerindoprilThe serum concentration of Theophylline can be decreased when it is combined with Perindopril.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Theophylline.Approved
PF-477736The therapeutic efficacy of PF-477736 can be decreased when used in combination with Theophylline.Investigational
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Theophylline.Withdrawn
PhenobarbitalThe metabolism of Theophylline can be increased when combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Theophylline can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PhosphoramidonThe serum concentration of Theophylline can be decreased when it is combined with Phosphoramidon.Experimental
PimozideThe metabolism of Pimozide can be decreased when combined with Theophylline.Approved
PioglitazoneThe metabolism of Theophylline can be decreased when combined with Pioglitazone.Approved, Investigational
Pipemidic acidThe metabolism of Theophylline can be decreased when combined with Pipemidic acid.Experimental
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Theophylline.Approved, Investigational
PirenzepineThe therapeutic efficacy of Pirenzepine can be decreased when used in combination with Theophylline.Approved
PirfenidoneThe serum concentration of Pirfenidone can be increased when it is combined with Theophylline.Approved, Investigational
Piromidic acidThe metabolism of Theophylline can be decreased when combined with Piromidic acid.Experimental
Polyestradiol phosphateThe serum concentration of Theophylline can be increased when it is combined with Polyestradiol phosphate.Approved
PomalidomideThe metabolism of Pomalidomide can be decreased when combined with Theophylline.Approved
PosaconazoleThe metabolism of Theophylline can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
Potassium IodideThe serum concentration of Theophylline can be increased when it is combined with Potassium Iodide.Approved
PrazepamThe therapeutic efficacy of Prazepam can be decreased when used in combination with Theophylline.Approved, Illicit
PraziquantelThe metabolism of Praziquantel can be decreased when combined with Theophylline.Approved, Vet Approved
PrimaquineThe metabolism of Primaquine can be decreased when combined with Theophylline.Approved
PrimidoneThe metabolism of Theophylline can be increased when combined with Primidone.Approved, Vet Approved
PrinomastatThe serum concentration of Theophylline can be decreased when it is combined with Prinomastat.Investigational
ProbenecidThe serum concentration of Theophylline can be increased when it is combined with Probenecid.Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Theophylline.Approved, Vet Approved
ProguanilThe metabolism of Proguanil can be decreased when combined with Theophylline.Approved
PromazineThe metabolism of Promazine can be decreased when combined with Theophylline.Approved, Vet Approved
PromestrieneThe serum concentration of Theophylline can be increased when it is combined with Promestriene.Investigational
PropafenoneThe serum concentration of Theophylline can be increased when it is combined with Propafenone.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Theophylline.Approved, Investigational, Vet Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Theophylline.Approved, Investigational
PropylthiouracilThe serum concentration of Theophylline can be increased when it is combined with Propylthiouracil.Approved
PrulifloxacinThe metabolism of Theophylline can be decreased when combined with Prulifloxacin.Investigational
PyrazinamideThe metabolism of Pyrazinamide can be decreased when combined with Theophylline.Approved
PyrimethamineThe metabolism of Theophylline can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuazepamThe therapeutic efficacy of Quazepam can be decreased when used in combination with Theophylline.Approved, Illicit
QuinaprilThe serum concentration of Theophylline can be decreased when it is combined with Quinapril.Approved, Investigational
QuinestrolThe serum concentration of Theophylline can be increased when it is combined with Quinestrol.Approved
QuinidineThe metabolism of Theophylline can be decreased when combined with Quinidine.Approved
QuinineThe serum concentration of Theophylline can be increased when it is combined with Quinine.Approved
RabeprazoleThe metabolism of Theophylline can be decreased when combined with Rabeprazole.Approved, Investigational
RacecadotrilThe serum concentration of Theophylline can be decreased when it is combined with Racecadotril.Investigational
RamelteonThe metabolism of Ramelteon can be decreased when combined with Theophylline.Approved, Investigational
RamiprilThe serum concentration of Theophylline can be decreased when it is combined with Ramipril.Approved
RanitidineThe metabolism of Ranitidine can be decreased when combined with Theophylline.Approved
RanolazineThe metabolism of Theophylline can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe metabolism of Rasagiline can be decreased when combined with Theophylline.Approved
RegadenosonTheophylline may decrease the vasodilatory activities of Regadenoson.Approved
RemikirenThe serum concentration of Theophylline can be decreased when it is combined with Remikiren.Approved
ResveratrolThe metabolism of Resveratrol can be decreased when combined with Theophylline.Approved, Experimental, Investigational
RifabutinThe metabolism of Theophylline can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Theophylline can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Theophylline can be increased when combined with Rifapentine.Approved
RiluzoleThe metabolism of Riluzole can be decreased when combined with Theophylline.Approved, Investigational
RiociguatTheophylline may increase the hypotensive activities of Riociguat.Approved
RitonavirThe metabolism of Theophylline can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Theophylline can be decreased when it is combined with Rivaroxaban.Approved
RizatriptanThe metabolism of Rizatriptan can be decreased when combined with Theophylline.Approved
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Theophylline.Investigational, Withdrawn
RolapitantThe metabolism of Theophylline can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Theophylline can be decreased when combined with Ropinirole.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Theophylline.Approved
RosiglitazoneThe metabolism of Theophylline can be decreased when combined with Rosiglitazone.Approved, Investigational
RosoxacinThe metabolism of Theophylline can be decreased when combined with Rosoxacin.Approved, Investigational
RotigotineThe metabolism of Rotigotine can be decreased when combined with Theophylline.Approved
RucaparibThe metabolism of Rucaparib can be decreased when combined with Theophylline.Approved, Investigational
RufloxacinThe metabolism of Theophylline can be decreased when combined with Rufloxacin.Experimental
S-3304The serum concentration of Theophylline can be decreased when it is combined with S-3304.Investigational
SaquinavirThe metabolism of Theophylline can be decreased when combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Theophylline can be decreased when it is combined with Saxagliptin.Approved
SecobarbitalThe metabolism of Theophylline can be increased when combined with Secobarbital.Approved, Vet Approved
SecoisolariciresinolThe serum concentration of Theophylline can be increased when it is combined with Secoisolariciresinol.Investigational
SelegilineThe metabolism of Selegiline can be decreased when combined with Theophylline.Approved, Investigational, Vet Approved
SertralineThe metabolism of Sertraline can be decreased when combined with Theophylline.Approved
SildenafilThe metabolism of Theophylline can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Theophylline can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Theophylline can be increased when it is combined with Simeprevir.Approved
SitafloxacinThe metabolism of Theophylline can be decreased when combined with Sitafloxacin.Experimental, Investigational
SitagliptinThe serum concentration of Theophylline can be decreased when it is combined with Sitagliptin.Approved, Investigational
SivelestatThe serum concentration of Theophylline can be decreased when it is combined with Sivelestat.Investigational
SJG-136The therapeutic efficacy of SJG-136 can be decreased when used in combination with Theophylline.Investigational
SolithromycinThe metabolism of Theophylline can be decreased when combined with Solithromycin.Investigational
SorafenibThe metabolism of Theophylline can be decreased when combined with Sorafenib.Approved, Investigational
SotalolSotalol may decrease the bronchodilatory activities of Theophylline.Approved
SparfloxacinThe metabolism of Theophylline can be decreased when combined with Sparfloxacin.Approved, Investigational
SpiraprilThe serum concentration of Theophylline can be decreased when it is combined with Spirapril.Approved
St. John's WortThe serum concentration of Theophylline can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Theophylline can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Theophylline can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Theophylline can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Theophylline can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
Synthetic Conjugated Estrogens, AThe serum concentration of Theophylline can be increased when it is combined with Synthetic Conjugated Estrogens, A.Approved
Synthetic Conjugated Estrogens, BThe serum concentration of Theophylline can be increased when it is combined with Synthetic Conjugated Estrogens, B.Approved
TacrineThe metabolism of Tacrine can be decreased when combined with Theophylline.Investigational, Withdrawn
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Theophylline.Approved
TelaprevirThe metabolism of Theophylline can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Theophylline can be decreased when combined with Telithromycin.Approved
TemafloxacinThe metabolism of Theophylline can be decreased when combined with Temafloxacin.Withdrawn
TemazepamThe therapeutic efficacy of Temazepam can be decreased when used in combination with Theophylline.Approved
TemocaprilThe serum concentration of Theophylline can be decreased when it is combined with Temocapril.Experimental, Investigational
Tenofovir disoproxilThe metabolism of Theophylline can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerbinafineThe metabolism of Theophylline can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TeriflunomideThe serum concentration of Theophylline can be decreased when it is combined with Teriflunomide.Approved
TertatololTertatolol may decrease the bronchodilatory activities of Theophylline.Experimental
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Theophylline.Approved, Investigational, Withdrawn
TheobromineThe metabolism of Theobromine can be decreased when combined with Theophylline.Approved, Investigational
ThiabendazoleThe metabolism of Theophylline can be decreased when combined with Thiabendazole.Approved, Vet Approved
ThiamylalThe serum concentration of Theophylline can be decreased when it is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe serum concentration of Theophylline can be decreased when it is combined with Thiopental.Approved, Vet Approved
ThioridazineThe metabolism of Theophylline can be decreased when combined with Thioridazine.Approved, Withdrawn
ThiorphanThe serum concentration of Theophylline can be decreased when it is combined with Thiorphan.Experimental
ThiothixeneThe metabolism of Thiothixene can be decreased when combined with Theophylline.Approved
Thyroid, porcineThe metabolism of Theophylline can be increased when combined with Thyroid, porcine.Approved
TiboloneThe serum concentration of Theophylline can be increased when it is combined with Tibolone.Approved, Investigational
TicagrelorThe metabolism of Theophylline can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Theophylline can be decreased when combined with Ticlopidine.Approved
TipranavirThe metabolism of Theophylline can be decreased when combined with Tipranavir.Approved, Investigational
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Theophylline.Approved
TocilizumabThe serum concentration of Theophylline can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Theophylline can be decreased when combined with Tolbutamide.Approved
TopiroxostatThe metabolism of Theophylline can be decreased when combined with Topiroxostat.Approved, Investigational
ToremifeneThe metabolism of Toremifene can be decreased when combined with Theophylline.Approved, Investigational
TrandolaprilThe serum concentration of Theophylline can be decreased when it is combined with Trandolapril.Approved
TranylcypromineThe metabolism of Theophylline can be decreased when combined with Tranylcypromine.Approved
TriamtereneThe metabolism of Triamterene can be decreased when combined with Theophylline.Approved
TriazolamThe therapeutic efficacy of Triazolam can be decreased when used in combination with Theophylline.Approved
TrifluoperazineThe metabolism of Trifluoperazine can be decreased when combined with Theophylline.Approved
TrimethoprimThe metabolism of Theophylline can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrovafloxacinThe metabolism of Theophylline can be decreased when combined with Trovafloxacin.Approved, Investigational, Withdrawn
TylosinThe metabolism of Theophylline can be decreased when combined with Tylosin.Vet Approved
UbenimexThe serum concentration of Theophylline can be decreased when it is combined with Ubenimex.Experimental, Investigational
UlinastatinThe serum concentration of Theophylline can be decreased when it is combined with Ulinastatin.Investigational
UlipristalThe metabolism of Ulipristal can be decreased when combined with Theophylline.Approved
VadimezanThe metabolism of Vadimezan can be decreased when combined with Theophylline.Investigational
Valproic AcidThe metabolism of Theophylline can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Theophylline can be decreased when combined with Valsartan.Approved, Investigational
VemurafenibThe serum concentration of Theophylline can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Theophylline can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Theophylline can be decreased when combined with Verapamil.Approved
VildagliptinThe serum concentration of Theophylline can be decreased when it is combined with Vildagliptin.Approved, Investigational
VoriconazoleThe metabolism of Theophylline can be decreased when combined with Voriconazole.Approved, Investigational
VoxilaprevirThe metabolism of Voxilaprevir can be decreased when combined with Theophylline.Approved
WarfarinThe metabolism of Warfarin can be decreased when combined with Theophylline.Approved
XimelagatranThe serum concentration of Theophylline can be decreased when it is combined with Ximelagatran.Approved, Investigational, Withdrawn
Z-Val-Ala-Asp fluoromethyl ketoneThe serum concentration of Theophylline can be decreased when it is combined with Z-Val-Ala-Asp fluoromethyl ketone.Experimental
ZafirlukastThe serum concentration of Zafirlukast can be decreased when it is combined with Theophylline.Approved, Investigational
ZeranolThe serum concentration of Theophylline can be increased when it is combined with Zeranol.Vet Approved
ZileutonThe serum concentration of Theophylline can be increased when it is combined with Zileuton.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Theophylline can be decreased when combined with Ziprasidone.Approved
ZofenoprilThe serum concentration of Theophylline can be decreased when it is combined with Zofenopril.Experimental
ZolmitriptanThe metabolism of Zolmitriptan can be decreased when combined with Theophylline.Approved, Investigational
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Theophylline.Approved
ZucapsaicinThe metabolism of Theophylline can be decreased when combined with Zucapsaicin.Approved
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Take with food.

References

Synthesis Reference

Nicolae S. Bodor, Kenneth B. Sloan, Yu-Neng Kuo, "Method for synthesizing certain selected pro-drug forms of theophylline." U.S. Patent US4000132, issued January, 1956.

US4000132
General References
Not Available
External Links
Human Metabolome Database
HMDB01889
KEGG Drug
D00371
KEGG Compound
C07130
PubChem Compound
2153
PubChem Substance
46505949
ChemSpider
2068
BindingDB
10847
ChEBI
28177
ChEMBL
CHEMBL190
Therapeutic Targets Database
DAP000002
PharmGKB
PA451647
IUPHAR
413
Guide to Pharmacology
GtP Drug Page
HET
TEP
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Theophylline
ATC Codes
R03DA54 — Theophylline, combinations excl. psycholepticsR03DA20 — Combinations of xanthinesR03DA74 — Theophylline, combinations with psycholepticsR03DA04 — TheophyllineR03DB04 — Theophylline and adrenergics
AHFS Codes
  • 86:16.00 — Respiratory Smooth Muscle Relaxants
PDB Entries
1eht / 1o15 / 2a3a / 3rox / 4eoh / 5mzj
FDA label
Download (85.2 KB)
MSDS
Download (75.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceMountain Sickness1
1CompletedBasic SciencePharmacokinetics2
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentHigh Altitude Pulmonary Hypertension1
1CompletedTreatmentMajor Depressive Disorder (MDD)1
1CompletedTreatmentProstate Neoplasms1
1RecruitingTreatmentAdvanced Solid Malignancies / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1WithdrawnTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancers1
1, 2CompletedPreventionPhysiological Function in Low Oxygen Environment1
1, 2CompletedTreatmentAcute Myelogenous Leukaemia (AML)1
2CompletedTreatmentAcute maxillary sinusitis caused by M. catarrhalis / Allergic Rhinitis (AR) / Asthma Bronchial1
2CompletedTreatmentAlbright Hereditary Osteodystrophy / Pseudohypoparathyroidism Type 1a1
2CompletedTreatmentLeukemias1
2Not Yet RecruitingTreatmentAlbright Hereditary Osteodystrophy / Pseudohypoparathyroidism1
2RecruitingTreatmentEnd Stage Renal Disease (ESRD) / Olfactory Disorders1
2, 3CompletedNot AvailableOther and unspecified effects of high altitude1
2, 3CompletedTreatmentAsthma Bronchial1
2, 3CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
2, 3CompletedTreatmentPrimary apnea of premature newborns1
2, 3Unknown StatusPreventionProphylaxis of Contrast-induced nephropathy1
3CompletedSupportive CarePulmonary Complications / Quality of Life / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedTreatmentAsthma Bronchial2
3CompletedTreatmentAsthma Bronchial / Chronic Lung Diseases1
3CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
4Active Not RecruitingTreatmentAsthma Bronchial1
4CompletedBasic ScienceHealthy Volunteers1
4CompletedHealth Services ResearchAsthma Bronchial1
4CompletedPreventionAdverse Effects / Contrast Induced Nephropathy (CIN) / Kidney Diseases / Renal Failure1
4CompletedTreatmentAsthma Bronchial1
4CompletedTreatmentBronchiectasis2
4CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
4RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD)1
Not AvailableCompletedNot AvailableChronic Obstructive Pulmonary Disease (COPD)1
Not AvailableCompletedBasic ScienceChronic Obstructive Pulmonary Disease (COPD)1
Not AvailableRecruitingNot AvailableChronic Obstructive Pulmonary Disease (COPD)1
Not AvailableRecruitingDevice FeasibilityHeart Ventricles1
Not AvailableUnknown StatusTreatmentChronic Obstructive Pulmonary Disease (COPD)1
Not AvailableUnknown StatusTreatmentFunction of Renal Transplant1

Pharmacoeconomics

Manufacturers
  • Fleming and co pharmaceuticals inc
  • Forest laboratories inc
  • Sanofi aventis us llc
  • Dm graham laboratories inc
  • Ucb inc
  • Whitby pharmaceuticals inc
  • Schwarz pharma inc
  • Schering corp
  • Central pharmaceuticals inc
  • Hospira inc
  • Inwood laboratories inc sub forest laboratories inc
  • Sandoz inc
  • Rp scherer north america div rp scherer corp
  • Ortho mcneil pharmaceutical inc
  • Schering corp sub schering plough corp
  • Fisons corp
  • Kv pharmaceutical co
  • Rp scherer north america
  • Hr cenci laboratories inc
  • Caraco pharmaceutical laboratories ltd
  • Lannett co inc
  • Panray corp sub ormont drug and chemical co inc
  • Alpharma us pharmaceuticals division
  • Cenci powder products inc
  • Halsey drug co inc
  • L perrigo co
  • Pharmaceutical assoc inc div beach products
  • Precision dose inc
  • Roxane laboratories inc
  • Taro pharmaceuticals usa inc
  • Wockhardt eu operations (swiss) ag
  • B braun medical inc
  • Baxter healthcare corp
  • 3m pharmaceuticals inc
  • Ferndale laboratories inc
  • Warner chilcott co llc
  • Monarch pharmaceuticals inc
  • Roerig div pfizer inc
  • Able laboratories inc
  • Glenmark generics ltd
  • Nostrum pharmaceuticals inc
  • Pliva inc
  • Pharmaceutical research assoc inc
  • Purdue pharmaceutical products lp
  • Graceway pharmaceuticals llc
  • Novartis consumer health inc
Packagers
Dosage forms
FormRouteStrength
Tablet, extended releaseOral100 mg
Tablet, extended releaseOral200 mg
Tablet, extended releaseOral300 mg
ElixirOral80 mg
LiquidOral80 mg/15mL
TabletOral
SyrupOral
Kit
Capsule, extended releaseOral100 mg
Capsule, extended releaseOral200 mg
Capsule, extended releaseOral300 mg
Capsule, extended releaseOral50 mg
Capsule, extended releaseOral100 mg/1
Capsule, extended releaseOral200 mg/1
Capsule, extended releaseOral300 mg/1
Capsule, extended releaseOral400 mg/1
Tablet, extended releaseOral450 mg
LiquidOral80 mg
Tablet, extended releaseOral250 mg
Tablet, extended releaseOral500 mg
TabletOral125 mg
TabletOral250 mg
SolutionOral80 mg/15mL
Tablet, extended releaseOral100 mg/1
Tablet, extended releaseOral200 mg/1
Tablet, extended releaseOral300 mg/1
Tablet, extended releaseOral450 mg/1
Tablet, extended releaseOral400 mg/1
Tablet, extended releaseOral600 mg/1
SolutionIntravenous
TabletOral300 mg/1
Injection, solutionIntravenous
Injection, solutionIntravenous160 mg/100mL
Injection, solutionIntravenous200 mg/100mL
Injection, solutionIntravenous320 mg/100mL
Injection, solutionIntravenous400 mg/100mL
Injection, solutionIntravenous80 mg/100mL
ElixirOral
TabletOral400 mg/1
TabletOral600 mg/1
Tablet, extended releaseOral400 mg
Tablet, extended releaseOral600 mg
Prices
Unit descriptionCostUnit
Elixophyllin GG 100-100 mg/15ml Solution 240ml Bottle60.98USD bottle
Uniphyl 600 mg 24 Hour tablet2.28USD tablet
Theo-24 400 mg 24 Hour Capsule2.04USD capsule
Theo-24 400 mg capsule sa1.97USD capsule
Uniphyl 400 mg 24 Hour tablet1.58USD tablet
Theo-24 300 mg 24 Hour Capsule1.45USD capsule
Theo-24 300 mg capsule sa1.4USD capsule
Theophylline 400 mg 24 Hour tablet1.27USD tablet
Theo-24 200 mg 24 Hour Capsule1.25USD capsule
Theo-24 200 mg capsule sa1.14USD capsule
Theochron 450 mg tablet sa0.94USD tablet
Theophylline CR 300 mg 12 Hour Capsule0.93USD capsule
Theo-24 100 mg 24 Hour Capsule0.83USD capsule
Theophylline CR 200 mg 12 Hour Capsule0.79USD capsule
Theophylline CR 450 mg 12 Hour tablet0.79USD tablet
Theo-24 100 mg capsule sa0.76USD capsule
Quibron 90-150 mg capsule0.73USD capsule
Theophylline CR 125 mg 12 Hour Capsule0.73USD capsule
Uniphyl 600 mg Sustained-Release Tablet0.68USD tablet
Uniphyl 400 mg Sustained-Release Tablet0.56USD tablet
Theochron 300 mg tablet sa0.54USD tablet
Theophylline CR 300 mg 12 Hour tablet0.51USD tablet
Theophylline CR 200 mg 12 Hour tablet0.4USD tablet
Theochron 200 mg tablet sa0.33USD tablet
Theophylline CR 100 mg 12 Hour tablet0.3USD tablet
Elixophyllin GG 100-100 mg/15ml Solution0.24USD ml
Theochron 100 mg tablet sa0.23USD tablet
Elixophyllin 80 mg/15ml Elixir0.2USD ml
Elixophyllin 80 mg/15 ml elix0.19USD ml
Apo-Theo La 300 mg Sustained-Release Tablet0.15USD tablet
Apo-Theo La 100 mg Sustained-Release Tablet0.14USD tablet
Apo-Theo La 200 mg Sustained-Release Tablet0.14USD tablet
Theophylline anhydrous powder0.08USD g
Theophylline 200 mg/100 ml d5w0.06USD ml
Theolair 5.3 mg/ml Liquid0.03USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)273 °CPhysProp
water solubility7360 mg/L (at 25 °C)YALKOWSKY,SH & HE,Y (2003)
logP-0.02HANSCH,C ET AL. (1995)
Caco2 permeability-4.35ADME Research, USCD
pKa8.81KORTUM,G ET AL (1961)
Predicted Properties
PropertyValueSource
Water Solubility22.9 mg/mLALOGPS
logP-0.26ALOGPS
logP-0.77ChemAxon
logS-0.9ALOGPS
pKa (Strongest Acidic)7.82ChemAxon
pKa (Strongest Basic)-0.78ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area69.3 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity44.93 m3·mol-1ChemAxon
Polarizability16.86 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9902
Caco-2 permeable+0.6172
P-glycoprotein substrateNon-substrate0.7281
P-glycoprotein inhibitor INon-inhibitor0.8939
P-glycoprotein inhibitor IINon-inhibitor0.911
Renal organic cation transporterNon-inhibitor0.8807
CYP450 2C9 substrateNon-substrate0.7738
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateNon-substrate0.5974
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9933
CYP450 2D6 inhibitorNon-inhibitor0.9827
CYP450 2C19 inhibitorNon-inhibitor0.9895
CYP450 3A4 inhibitorNon-inhibitor0.9616
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9956
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9447
BiodegradationReady biodegradable0.5942
Rat acute toxicity2.7898 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8819
hERG inhibition (predictor II)Non-inhibitor0.8927
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (2.96 KB)
Spectra
SpectrumSpectrum TypeSplash Key
GC-MS Spectrum - GC-MS (1 TMS)GC-MSsplash10-0f79-6970000000-224461ad62a44dbdf860
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-001j-7900000000-a08735d528e738752429
GC-MS Spectrum - CI-BGC-MSsplash10-001i-0900000000-d0882f7d959c726e7623
GC-MS Spectrum - EI-BGC-MSsplash10-001i-9700000000-8d0e1898a6571fbca10a
GC-MS Spectrum - GC-MSGC-MSsplash10-0f79-6970000000-224461ad62a44dbdf860
Mass Spectrum (Electron Ionization)MSsplash10-00lr-9500000000-2c8464c2fe84464c207f
MS/MS Spectrum - Quattro_QQQ 10V, Positive (Annotated)LC-MS/MSsplash10-00di-0900000000-0092516012d6a2a93b31
MS/MS Spectrum - Quattro_QQQ 25V, Positive (Annotated)LC-MS/MSsplash10-00di-4900000000-dcf52c18a6996f412b1a
MS/MS Spectrum - Quattro_QQQ 40V, Positive (Annotated)LC-MS/MSsplash10-00kf-9000000000-09089337909892ef44cb
MS/MS Spectrum - EI-B (Unknown) , PositiveLC-MS/MSsplash10-001j-7900000000-a08735d528e738752429
MS/MS Spectrum - CI-B (Unknown) , PositiveLC-MS/MSsplash10-001i-0900000000-d0882f7d959c726e7623
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, NegativeLC-MS/MSsplash10-004i-0900000000-c4943571126a44bb9e5a
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, NegativeLC-MS/MSsplash10-004i-0900000000-bc12ce29acd02fa749b8
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, NegativeLC-MS/MSsplash10-03k9-0900000000-d63f60043f186fbb9bc0
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, NegativeLC-MS/MSsplash10-070l-4900000000-d293ab2fa6199dbaf97a
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, NegativeLC-MS/MSsplash10-05ru-9400000000-dde4775588d52c83806f
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, NegativeLC-MS/MSsplash10-004i-0900000000-556e382f583d610ef1f0
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, NegativeLC-MS/MSsplash10-004i-0900000000-89e34f5158856ba33469
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, NegativeLC-MS/MSsplash10-03k9-0900000000-65a6897d72954e875b00
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, NegativeLC-MS/MSsplash10-070l-4900000000-df16604bd6c40cee8f24
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, NegativeLC-MS/MSsplash10-05r3-9500000000-39a721dcecc86ed95507
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, PositiveLC-MS/MSsplash10-001i-1900000000-e67ff7ef9a955b90eb3f
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, PositiveLC-MS/MSsplash10-001i-3900000000-1870952d98dbba22ace8
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, PositiveLC-MS/MSsplash10-00di-7900000000-dc0e9606776c43a7823f
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, PositiveLC-MS/MSsplash10-014j-9300000000-2c4c6490dda3ed3b563f
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, PositiveLC-MS/MSsplash10-014i-9000000000-26a6c0c23a465afdcde1
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, PositiveLC-MS/MSsplash10-01q9-1900000000-b11ca3441bb29fef1906
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, PositiveLC-MS/MSsplash10-0002-9400000000-63726fe0b49a9dc6ba7e
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, PositiveLC-MS/MSsplash10-00di-9100000000-139f765bc9b5855960c6
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, PositiveLC-MS/MSsplash10-00di-9000000000-88b5cb393b960973ac64
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, PositiveLC-MS/MSsplash10-00yi-9000000000-1ebbddce3c7133972546
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - DI-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-004i-0900000000-f85319d9f010d9331358
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-004i-0900000000-aa13286b9e614fd8fe53
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-004i-0900000000-e15e11a3656aeeab5cd9
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-03mi-0900000000-2a03f291514704faa75f
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-03k9-2900000000-ab88f9462f7fd47e2cdb
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-02il-5900000000-10615507746dde65941c
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-016r-9300000000-23b6aaf5dc6055695076
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-9100000000-0cbbbe667a26bdb5e69c
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-9000000000-ae6306e2b4613a843262
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-004i-0900000000-c4943571126a44bb9e5a
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-004i-0900000000-bc12ce29acd02fa749b8
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-03k9-0900000000-024b4b169aaa17d8a74e
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-070l-4900000000-d293ab2fa6199dbaf97a
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-05ru-9400000000-dde4775588d52c83806f
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-004i-0900000000-556e382f583d610ef1f0
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-004i-0900000000-89e34f5158856ba33469
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-03k9-0900000000-65a6897d72954e875b00
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-070l-4900000000-983504ecebbfb75b5084
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-05r3-9500000000-39a721dcecc86ed95507
LC-MS/MS Spectrum - LC-ESI-IT , negativeLC-MS/MSsplash10-03fr-0900000000-301f6a6c606c9a7b0a70
MS/MS Spectrum - Linear Ion Trap , negativeLC-MS/MSsplash10-03di-0900000000-605dffad97fe00830afb
MS/MS Spectrum - Linear Ion Trap , negativeLC-MS/MSsplash10-03di-0900000000-a555f5610ea0cc93fb51
MS/MS Spectrum - , negativeLC-MS/MSsplash10-004i-0900000000-f549c20fef4bb5ca418e
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-004i-0900000000-f1e7ed4d06480c676ae5
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0089-0900000000-b98ed10778362fb92f0f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-0900000000-da2d25abcc877a840ad2
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-0900000000-abde646c11db3466840e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0089-0900000000-dbb621bedc8cfcd20c79
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-2900000000-90c98019c1e8f7da070b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-7900000000-cb3893a87548cb64cf27
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-01ba-9400000000-0063418efb7894950690
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-9100000000-f981abb3cf2d588f83ed
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-9100000000-f0fbdf55d630257724bf
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0gb9-9000000000-fe69541c14c87da8c124
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-001i-1900000000-e67ff7ef9a955b90eb3f
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-001i-3900000000-1870952d98dbba22ace8
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00di-7900000000-b5c4010c670127e11063
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014j-9300000000-2c4c6490dda3ed3b563f
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-014i-9000000000-26a6c0c23a465afdcde1
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-01q9-1900000000-c1f0683d1932a6c393f8
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0002-9400000000-63726fe0b49a9dc6ba7e
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00di-9100000000-139f765bc9b5855960c6
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00di-9000000000-88b5cb393b960973ac64
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00yi-9000000000-a92e0f58a066f6e1c88b
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-001i-0900000000-08f49d05e8c651dd89ec
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00di-1900000000-bad7ec3fbdf7e1eecae4
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-01ba-9500000000-fadd3d94aac67bb5574b
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-9200000000-426452757fca6f6b9b76
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-9100000000-52e441104cd15fca9363
MS/MS Spectrum - Linear Ion Trap , positiveLC-MS/MSsplash10-00di-0900000000-d8a03644c7ee59de6416
MS/MS Spectrum - Linear Ion Trap , positiveLC-MS/MSsplash10-00di-0900000000-6016ebc9f342f37971a7
MS/MS Spectrum - Linear Ion Trap , positiveLC-MS/MSsplash10-03di-0930000000-7539c4c857812dd013e7
MS/MS Spectrum - Linear Ion Trap , positiveLC-MS/MSsplash10-03di-0930000000-17caee7404f50a2538bb
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001i-1900000000-d5c161725a650cbeb97c
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00di-2910000000-c9eb85b2c5aaf500073c
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001i-0900000000-08b71a19d1a98ad63f16
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-0900000000-cc9a16a03fd1ddcf16ce
1H NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

Description
This compound belongs to the class of organic compounds known as xanthines. These are purine derivatives with a ketone group conjugated at carbons 2 and 6 of the purine moiety.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Imidazopyrimidines
Sub Class
Purines and purine derivatives
Direct Parent
Xanthines
Alternative Parents
6-oxopurines / Alkaloids and derivatives / Pyrimidones / Vinylogous amides / Imidazoles / Heteroaromatic compounds / Ureas / Lactams / Azacyclic compounds / Organopnictogen compounds
show 4 more
Substituents
Xanthine / 6-oxopurine / Purinone / Alkaloid or derivatives / Pyrimidone / Pyrimidine / Azole / Imidazole / Heteroaromatic compound / Vinylogous amide
show 11 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
dimethylxanthine (CHEBI:28177) / Purine alkaloids (C07130) / a small molecule (CPD-12479)

Targets

Details
1. Adenosine receptor A1
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Purine nucleoside binding
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
ADORA1
Uniprot ID
P30542
Uniprot Name
Adenosine receptor A1
Molecular Weight
36511.325 Da
References
  1. Nantwi KD, Basura GJ, Goshgarian HG: Adenosine A1 receptor mRNA expression and the effects of systemic theophylline administration on respiratory function 4 months after C2 hemisection. J Spinal Cord Med. 2003 Winter;26(4):364-71. [PubMed:14992338]
  2. Daly JW, Jacobson KA, Ukena D: Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63. [PubMed:3588607]
Details
2. Adenosine receptor A2a
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Identical protein binding
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name
ADORA2A
Uniprot ID
P29274
Uniprot Name
Adenosine receptor A2a
Molecular Weight
44706.925 Da
References
  1. Pechlivanova DM, Georgiev VP: Effects of single and long-term theophylline treatment on the threshold of mechanical nociception: contribution of adenosine A1 and alpha2-adrenoceptors. Methods Find Exp Clin Pharmacol. 2005 Nov;27(9):659-64. [PubMed:16357952]
  2. Daly JW, Jacobson KA, Ukena D: Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63. [PubMed:3588607]
Details
3. Adenosine receptor A2b
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
G-protein coupled adenosine receptor activity
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name
ADORA2B
Uniprot ID
P29275
Uniprot Name
Adenosine receptor A2b
Molecular Weight
36332.655 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Philipp S, Yang XM, Cui L, Davis AM, Downey JM, Cohen MV: Postconditioning protects rabbit hearts through a protein kinase C-adenosine A2b receptor cascade. Cardiovasc Res. 2006 May 1;70(2):308-14. Epub 2006 Feb 23. [PubMed:16545350]
  3. Phelps PT, Anthes JC, Correll CC: Characterization of adenosine receptors in the human bladder carcinoma T24 cell line. Eur J Pharmacol. 2006 Apr 24;536(1-2):28-37. Epub 2006 Mar 3. [PubMed:16581066]
  4. Fozard JR, Baur F, Wolber C: Antagonist pharmacology of adenosine A2B receptors from rat, guinea pig and dog. Eur J Pharmacol. 2003 Aug 15;475(1-3):79-84. [PubMed:12954362]
  5. Holgate ST: The Quintiles Prize Lecture 2004. The identification of the adenosine A2B receptor as a novel therapeutic target in asthma. Br J Pharmacol. 2005 Aug;145(8):1009-15. [PubMed:15980878]
  6. Daly JW, Jacobson KA, Ukena D: Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63. [PubMed:3588607]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in mediating central nervous system effects of therapeutic agents ranging f...
Gene Name
PDE4B
Uniprot ID
Q07343
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Molecular Weight
83342.695 Da
References
  1. Lipworth BJ: Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease. Lancet. 2005 Jan 8-14;365(9454):167-75. [PubMed:15639300]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:9714779, ...
Gene Name
PDE5A
Uniprot ID
O76074
Uniprot Name
cGMP-specific 3',5'-cyclic phosphodiesterase
Molecular Weight
99984.14 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name
PDE4A
Uniprot ID
P27815
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Molecular Weight
98142.155 Da
References
  1. Wang K, Chen JQ, Chen Z, Chen JC: Inhibition of human phosphodiesterase 4A expressed in yeast cell GL62 by theophylline, rolipram, and acetamide-45. Acta Pharmacol Sin. 2002 Nov;23(11):1013-7. [PubMed:12421478]
  2. Haider S: Cyclic AMP level and phosphodiesterase activity during 17alpha,20beta-dihydroxy-4-pregnen-3-one induction and theophylline inhibition of oocyte maturation in the catfish, Clarias batrachus. Comp Biochem Physiol A Mol Integr Physiol. 2003 Feb;134(2):267-74. [PubMed:12547256]
  3. Rickards KJ, Andrews MJ, Waterworth TH, Alexander GB, Cunningham FM: Differential effects of phosphodiesterase inhibitors on platelet activating factor (PAF)- and adenosine diphosphate (ADP)-induced equine platelet aggregation. J Vet Pharmacol Ther. 2003 Aug;26(4):277-82. [PubMed:12887610]
  4. Usta C, Sadan G, Tuncel B: The effect of the indomethacin on phosphodiesterase inhibitors mediated responses in isolated trachea preparations. Prostaglandins Leukot Essent Fatty Acids. 2004 Sep;71(3):137-41. [PubMed:15253881]
  5. Lee JM, Zemans RL, Hejazi M, Chin BB, Ladenson PW, Caturegli P: Modulation of thyroidal radioiodine uptake by theophylline. Exp Mol Pathol. 2004 Oct;77(2):116-20. [PubMed:15351234]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
Gene Name
PDE3A
Uniprot ID
Q14432
Uniprot Name
cGMP-inhibited 3',5'-cyclic phosphodiesterase A
Molecular Weight
124978.06 Da
References
  1. Rickards KJ, Andrews MJ, Waterworth TH, Alexander GB, Cunningham FM: Differential effects of phosphodiesterase inhibitors on platelet activating factor (PAF)- and adenosine diphosphate (ADP)-induced equine platelet aggregation. J Vet Pharmacol Ther. 2003 Aug;26(4):277-82. [PubMed:12887610]
  2. Wu BN, Lin RJ, Lo YC, Shen KP, Wang CC, Lin YT, Chen IJ: KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-14. Epub 2004 Jul 5. [PubMed:15237094]
  3. Kajikawa S, Kigami D, Nakayama H, Doi K: Changes in submaxillary gland gene expression in F344 rats by multiple dosing of theophylline. Exp Anim. 2006 Apr;55(2):143-6. [PubMed:16651698]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Activator
General Function
Transcription factor binding
Specific Function
Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an impo...
Gene Name
HDAC2
Uniprot ID
Q92769
Uniprot Name
Histone deacetylase 2
Molecular Weight
55363.855 Da
References
  1. Ito K, Lim S, Caramori G, Cosio B, Chung KF, Adcock IM, Barnes PJ: A molecular mechanism of action of theophylline: Induction of histone deacetylase activity to decrease inflammatory gene expression. Proc Natl Acad Sci U S A. 2002 Jun 25;99(13):8921-6. Epub 2002 Jun 17. [PubMed:12070353]
  2. Cosio BG, Tsaprouni L, Ito K, Jazrawi E, Adcock IM, Barnes PJ: Theophylline restores histone deacetylase activity and steroid responses in COPD macrophages. J Exp Med. 2004 Sep 6;200(5):689-95. Epub 2004 Aug 30. [PubMed:15337792]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Calcium-dependent phospholipid-binding protein that plays a role in calcium-mediated intracellular processes (PubMed:14674885). Involved in the TNF-alpha receptor signaling pathway in a calcium-dependent manner (PubMed:14674885). Exhibits calcium-dependent phospholipid binding properties (PubMed:9430674, PubMed:19539605). Plays a role in neuronal progenitor cell differentiation; induces neurite outgrowth via a AKT-dependent signaling cascade and calcium-independent manner (PubMed:23263657, PubMed:25450385). May recruit target proteins to the cell membrane in a calcium-dependent manner (PubMed:12522145). May function in membrane trafficking (PubMed:9430674). Involved in TNF-alpha-induced NF-kappa-B transcriptional repression by inducing endoprotease processing of the transcription factor NF-kappa-B p65/RELA subunit (PubMed:18212740). Also induces endoprotease processing of NF-kappa-B p50/NFKB1, p52/NFKB2, RELB and REL (PubMed:18212740).
Specific Function
Calcium ion binding
Gene Name
CPNE1
Uniprot ID
Q99829
Uniprot Name
Copine-1
Molecular Weight
59058.34 Da
References
  1. Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [PubMed:18951874]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Catalyzes intramembrane proteolysis of some signal peptides after they have been cleaved from a preprotein, resulting in the release of the fragment from the ER membrane into the cytoplasm. Required to generate lymphocyte cell surface (HLA-E) epitopes derived from MHC class I signal peptides (PubMed:11714810). May be necessary for the removal of the signal peptide that remains attached to the hepatitis C virus core protein after the initial proteolytic processing of the polyprotein (PubMed:12145199). Involved in the intramembrane cleavage of the integral membrane protein PSEN1 (PubMed:12077416, PubMed:11714810, PubMed:14741365). Cleaves the integral membrane protein XBP1 isoform 1 in a DERL1/RNF139-dependent manner (PubMed:25239945). May play a role in graft rejection (By similarity).
Specific Function
Aspartic endopeptidase activity, intramembrane cleaving
Gene Name
HM13
Uniprot ID
Q8TCT9
Uniprot Name
Minor histocompatibility antigen H13
Molecular Weight
41487.86 Da
References
  1. Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [PubMed:18951874]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
May antagonize Nodal signaling.
Specific Function
Carbohydrate binding
Gene Name
NOMO1
Uniprot ID
Q15155
Uniprot Name
Nodal modulator 1
Molecular Weight
134323.005 Da
References
  1. Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [PubMed:18951874]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
Gene Name
PARP1
Uniprot ID
P09874
Uniprot Name
Poly [ADP-ribose] polymerase 1
Molecular Weight
113082.945 Da
References
  1. Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [PubMed:18951874]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Promotes functional expression of homomeric alpha-7 and alpha-8 nicotinic acetylcholine receptors at the cell surface. May also promote functional expression of homomeric serotoninergic 5-HT3 receptors, and of heteromeric acetylcholine receptors alpha-3/beta-2, alpha-3/beta-4, alpha-4/beta-2 and alpha-4/beta-4.
Specific Function
Acetylcholine receptor binding
Gene Name
RIC3
Uniprot ID
Q7Z5B4
Uniprot Name
Protein RIC-3
Molecular Weight
41091.77 Da
References
  1. Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [PubMed:18951874]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Monoglycylase which modifies alpha- and beta-tubulin, generating side chains of glycine on the gamma-carboxyl groups of specific glutamate residues within the C-terminal tail of alpha- and beta-tubulin. Involved in the side-chain initiation step of the glycylation reaction by adding a single glycine chain to generate monoglycine side chains. Not involved in elongation step of the polyglycylation reaction.
Specific Function
Atp binding
Gene Name
TTLL3
Uniprot ID
Q9Y4R7
Uniprot Name
Tubulin monoglycylase TTLL3
Molecular Weight
87413.395 Da
References
  1. Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [PubMed:18951874]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Brosen K: Drug interactions and the cytochrome P450 system. The role of cytochrome P450 1A2. Clin Pharmacokinet. 1995;29 Suppl 1:20-5. [PubMed:8846619]
  2. Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [PubMed:19754423]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  4. Sarkar MA, Hunt C, Guzelian PS, Karnes HT: Characterization of human liver cytochromes P-450 involved in theophylline metabolism. Drug Metab Dispos. 1992 Jan-Feb;20(1):31-7. [PubMed:1346993]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Zinc ion binding
Specific Function
Catalyzes the hydrolytic deamination of adenosine and 2-deoxyadenosine. Plays an important role in purine metabolism and in adenosine homeostasis. Modulates signaling by extracellular adenosine, an...
Gene Name
ADA
Uniprot ID
P00813
Uniprot Name
Adenosine deaminase
Molecular Weight
40764.13 Da
References
  1. Saboury AA, Bagheri S, Ataie G, Amanlou M, Moosavi-Movahedi AA, Hakimelahi GH, Cristalli G, Namaki S: Binding properties of adenosine deaminase interacted with theophylline. Chem Pharm Bull (Tokyo). 2004 Oct;52(10):1179-82. [PubMed:15467230]
  2. Singh LS, Sharma R: Purification and characterization of intestinal adenosine deaminase from mice. Mol Cell Biochem. 2000 Jan;204(1-2):127-34. [PubMed:10718633]
  3. Bandyopadhyay BC, Poddar MK: Theophylline-induced changes in mammalian adenosine deaminase activity and corticosterone status: possible relation to immune response. Methods Find Exp Clin Pharmacol. 1997 Apr;19(3):181-4. [PubMed:9203166]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Sarkar MA, Hunt C, Guzelian PS, Karnes HT: Characterization of human liver cytochromes P-450 involved in theophylline metabolism. Drug Metab Dispos. 1992 Jan-Feb;20(1):31-7. [PubMed:1346993]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d 24-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulf...
Gene Name
SLC22A7
Uniprot ID
Q9Y694
Uniprot Name
Solute carrier family 22 member 7
Molecular Weight
60025.025 Da
References
  1. Kobayashi Y, Sakai R, Ohshiro N, Ohbayashi M, Kohyama N, Yamamoto T: Possible involvement of organic anion transporter 2 on the interaction of theophylline with erythromycin in the human liver. Drug Metab Dispos. 2005 May;33(5):619-22. Epub 2005 Feb 11. [PubMed:15708966]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34